Ludwig Institute for Cancer Research, Old Road Campus Research Building, Roosevelt Drive, Oxford.
Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
Nat Rev Mol Cell Biol. 2017 Apr;18(4):246-262. doi: 10.1038/nrm.2016.143. Epub 2017 Jan 5.
Bromodomains (BRDs) are evolutionarily conserved protein-protein interaction modules that are found in a wide range of proteins with diverse catalytic and scaffolding functions and are present in most tissues. BRDs selectively recognize and bind to acetylated Lys residues - particularly in histones - and thereby have important roles in the regulation of gene expression. BRD-containing proteins are frequently dysregulated in cancer, they participate in gene fusions that generate diverse, frequently oncogenic proteins, and many cancer-causing mutations have been mapped to the BRDs themselves. Importantly, BRDs can be targeted by small-molecule inhibitors, which has stimulated many translational research projects that seek to attenuate the aberrant functions of BRD-containing proteins in disease.
溴结构域（BRDs）是进化上保守的蛋白-蛋白相互作用模块，存在于具有多种催化和支架功能的广泛蛋白质中，并且存在于大多数组织中。BRD 特异性识别和结合乙酰化的 Lys 残基 - 特别是在组蛋白中 - 并因此在基因表达的调控中发挥重要作用。BRD 包含的蛋白质在癌症中经常失调，它们参与产生多种，通常致癌的蛋白质的基因融合，并且许多致癌突变已映射到 BRD 本身。重要的是，BRD 可以被小分子抑制剂靶向，这激发了许多转化研究项目，旨在减轻疾病中 BRD 包含的蛋白质的异常功能。
